851202-78-3Relevant academic research and scientific papers
The use of formamidine protection for the derivatization of aminobenzoic acids
Zhichkin, Paul E.,Peterson, Lisa H.,Beer, Catherine M.,Rennells, W. Martin
supporting information; experimental part, p. 8954 - 8959 (2009/04/11)
(Chemical Equation Presented) N,N-Dimethylformamidine and novel N,N-diisopropylformamidine protecting groups were used to carry out a one-pot conversion of aminobenzoic acids into the corresponding amides. General conditions for an in situ transformation of aminobenzoic acids and their heterocyclic analogues into the corresponding formamidine-protected acid chlorides were developed. These chlorides were used in reactions with amines, including poorly reactive anilines. The protected amides were then smoothly deprotected by heating with ethylenediamine derivatives, resulting in a general procedure for the one-pot transformation of aminobenzoic acids into their amides. Our one-pot procedure was successfully applied to the preparation of several compounds of pharmaceutical interest.
PRO-DRUGS OF N-THIAZOL-2YL-BENZAMIDE DERIVATIVES
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Page/Page column 37, (2010/11/24)
The invention relates to compounds of the formula I wherein the variables are as defined in the claims. The compounds are pro-drugs of A2A-receptor ligands with improved aqueous solubility, and are useful in the treatment of neurological and psychiatric disorders where an A2A-receptor is implicated.
N-THIAZOL-2-YL-BENZAMIDE DERIVATIVES
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Page/Page column 25, (2008/06/13)
The invention relates to N-thiazol-2-yl-benzamide derivatives of the formula I in the description wherein the variables are as defined in the claims. The compounds are A2A-receptor ligands, such as antagonists, agonists, reverse agonists or partial agonists, and are useful in the treatment of neurological and psychiatric disorders where an A2A-receptor is implicated.
